Assay Detail
Binding
CHEMBL847754
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against sigma receptor using radioligand ([3H](+)-pentazocine) binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.03 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346409 | — | — | 1 | 9.30 |
| CHEMBL140054 | — | — | 1 | 8.07 |
| CHEMBL143407 | — | — | 1 | 8.07 |
| CHEMBL26320 | — | — | 1 | 7.77 |
| CHEMBL143750 | — | — | 1 | 6.96 |
| CHEMBL102119 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346409 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL140054 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL143407 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL26320 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL143750 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL102119 | — | IC50 | > | 10000.0 | nM | - |